双环分子
环加成
组合化学
药物发现
化学
有机化学
催化作用
生物化学
作者
Yujie Liang,Ronewa Nematswerani,Constantin G. Daniliuc,Frank Glorius
标识
DOI:10.1002/anie.202402730
摘要
Synthesis of bicyclic scaffolds has emerged as an important research topic in modern drug development because they can serve as saturated bioisosters to enhance the physicochemical properties and metabolic profiles of drug candidates. Here we report a remarkably simple silver‐enabled strategy to access polysubstituted 3‐azabicyclo[3.1.1]heptanes in a single operation from readily accessible bicyclo[1.1.0]butanes (BCBs) and isocyanides. The process is proposed to involve a formal [3+3]/[3+2]/retro‐[3+2] cycloaddition sequence. This novel protocol allows for rapid generation of molecular complexity from simple starting materials, and the products can be easily derivatized, further enriching the BCB cycloaddition chemistry and the growing set of valuable sp3‐rich bicyclic building blocks.
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